Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Abstract

The aims of the present study were to investigate the skin permeation and cellular uptake of a microemulsion (ME) containing total flavone of rhizoma arisaematis (TFRA), and to evaluate its effects on skin structure. Pseudo-ternary phase diagrams were constructed to evaluate ME regions with various surfactants and cosurfactants. Eight formulations of oil-in-water MEs were selected as vehicles, and in vitro skin-permeation experiments were performed to optimize the ME formulation and to evaluate its permeability, in comparison to that of an aqueous suspension. Laser scanning confocal microscopy and fluorescent-activated cell sorting were used to explore the cellular uptake of rhodamine 110-labeled ME in human epidermal keratinocytes (HaCaT) and human embryonic skin fibroblasts (CCC-ESF-1). The structure of stratum corneum treated with ME was observed using a scanning electron microscope. Furthermore, skin irritation was tested to evaluate the safety of ME. ME formulated with 4% ethyl oleate (weight/weight), 18% Cremophor EL ® (weight/weight), and 18% Transcutol ® P, with 1% Azone to enhance permeation, showed good skin permeability. ME-associated transdermal fluxes of schaftoside and isoschaftoside, two major effective constituents of TFRA, were 3.72-fold and 5.92-fold higher, respectively, than those achieved using aqueous suspensions. In contrast, in vitro studies revealed that uptake by HaCaT and CCC-ESF-1 cells was lower with ME than with an aqueous suspension. Stratum corneum loosening and shedding was observed in nude mouse skin treated with ME, although ME produced no observable skin irritation in rabbits. These findings indicated that ME enhanced transdermal TFRA delivery effectively and showed good biocompatibility with skin tissue.

Preparation and evaluation of microemulsion-based transdermal delivery of Cistanche tubulosa phenylethanoid glycosides

“…The permeation rate of ME5 (86.795±0.23 µg/cm −2 /h −1 ) was significantly increased compared with the permeation rates of ME1 (69.57±0.78, P=0.0094), ME2 (44.326±0.84, P=0.0052), ME3 (79.859±0.12, P=0.039) and ME4 (58.332±0.39 µg/cm −2 /h −1 , P=0.0063, Fig. 5; Table III) This was consistent with the results of a previous study, in which the thermodynamic activity of the ME drug cargo may decrease with the increase of surfactant levels (12,28). The viscosity of ME5 (30.43±0.12 mPa.s) was lower compared with the other ME1 (80.51±0.87 mPa.s, P=0.0076), ME2 (47.52±0.54 mPa.s, P=0.0089), ME3 (60.49±1.34 mPa.s, P=0.0094) and ME4 (43.27±0.21 mPa.s, P=0.0059).…”

“…To obtain a concentration range of components for the existing microemulsion boundary, pseudoternary phase diagrams were constructed using a water titration method as previously described (12). Three phase diagrams were prepared with 1:3, 1:1, and 3:1 weight ratios of surfactant to cosurfactant.…”

“…Permeation experiments were conducted as previously described (12). The excised skin was clamped between the donor and the receptor chamber of a vertical diffusion cell with an effective diffusion area of 2.8 cm 2 .…”

Nanostructured lipid carriers for percutaneous administration of alkaloids isolated from Aconitum sinomontanum

“…Rats were anesthetized, euthanized, their abdominal fur was removed with a razor, and then the skin was excised carefully and washed with normal saline. In vitro permeation experiments were conducted using a Franz diffusion cell (Fulansi Electronic Science and Trade Co, Ltd, Tianjin, China) fitted with excised rat skin [ 37 ]. Each donor compartment had a diffusion area of 2.0 cm 2 and each receptor compartment was filled with 12.5 mL of freshly prepared normal saline containing 20% PEG 400 (v/v) to provide sink conditions [ 38 ].…”

Foray into Concepts of Design and Evaluation of Microemulsions as a Modern Approach for Topical Applications in Acne Pathology

“…Furthermore, O/W microemulsions for dermal and transdermal delivery with a 2% flavone extract of rhizoma arisaematis with analgesic properties were formulated using a vehicle composed of a S/CoS mixture with Cremophor EL 9-27% and Transcutol 8-27% with stabilizing properties for ethyl oleate particles 4-8% in a medium of 60% water. TEM analysis revealed the presence of spherical particles of oil phase with a dimension under 100 nm, stabilized in the aqueous medium [190].…”